Volume 4 - Issue 4 (In Press 2018)                   Back to the articles list | Back to browse issues page

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Department of Natural Active Principles and Toxicology, School of Pharmaceutical Sciences, UNESP- Univ Estadual Paulista, Araraquara, Sao Paulo, Brazil
Abstract:   (48 Views)
Trypanosomiasis currently has only two drugs for the treatment: benznidazole and nifurtimox. Studies have indicated ursolic acid activity on trypomastigotes and intracellular amastigotes of T. cruzi and these findings create expectations for its potential therapeutic use in the trypanosomiasis treatment. Therapeutic application of a compound requires the investigation of its pharmacokinetic properties in order to obtain relevant information to design the in vivo assays and the dose regimen. This study was conducted to evaluate the pharmacokinetic profile of ursolic acid administered to Wistar rats at different doses and routes (intravenously; 1mg / kg and orally; 20 and 50 mg / kg). The oral bioavailability (Foral) was significantly different among groups that received different doses, 2.8% for 20 mg/kg and 1.55% for 50 mg/kg, and this result suggests the interference of the poor water solubility of ursolic acid on its absorption process. The pharmacokinetic parameters related to the distribution and elimination were similar, which allows us to infer that in this dose range there is no saturation in these process and the kinetics is linear. The pharmacokinetic properties of ursolic acid observed in this study indicate that the improvement of its water solubility throught pharmacotechnical resources are of great utility for its oral bioavailability and the development of a product with potential therapeutic application. This new pharmaceutical formulation may be used for future studies on the therapeutic properties of the compound administered orally.
     
Type of Study: Research | Subject: Pharmacology

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